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- W2021583585 abstract "The binding profiles of SA4503 (1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride), a novel σ receptor ligand, to σ1 and σ2 receptor subtypes in guinea pig and rat brain membranes were evaluated. SA4503 showed a high affinity for the σ1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 ± 1.9 nM), while it had about 100-fold less affinity for the σ2 receptor subtype labeled by [3H]1,3-di(2-tolyl)guanidine ([3H]DTG) in the presence of 200 nM (+)-pentazocine. SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. The inhibition curves of SA4503 for (+)-[3H]pentazocine binding were shifted to the right in the presence of guanosine 5′-o-(3-thiotriphosphate) (GTPγS), as similar to those of (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3-PPP) and (+)-pentazocine, σ1 receptor agonists. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. These results indicated that SA4503 is a potent and selective agonist for the σ1 receptor subtype in the brain. In addition, SA4503 inhibited specific (+)-[3H]pentazocine binding in a competitive manner." @default.
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- W2021583585 date "1996-06-01" @default.
- W2021583585 modified "2023-09-26" @default.
- W2021583585 title "Binding properties of SA4503, a novel and selective σ1 receptor agonist" @default.
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- W2021583585 doi "https://doi.org/10.1016/0014-2999(96)00201-4" @default.
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